This invention relates to a composition whereby fluid, nonaqueous, defoaming or antifoaming compositions are prepared as relatively free flowing granular combinates by intermixing them with a low density, highly porous, generally spherical, water soluble carbohydrate-based agglomerate such as maltodextrin to form adjuvant agglomerate combinates suitable for addition to products or processes wherever a rapid dispersion of the antifoaming or defoaming compound in an aqueous medium is indicated or desired.
The following listing and characterization of fluid, nonaqueous, antifoaming or defoaming compositions or compounds used in the practice of this invention is given to more precisely and particularly illustrate applicable compositions and compounds. The listing is not meant to limit or to specifically define the category of fluid, nonaqueous antifoaming or defoaming compositions, but rather to illustrate the scope of compositions applicable to the formation of the adjuvant agglomerate combinates.
Fluid hydrocarbon oil-based antifoaming or defoaming compositions containing a hydrocarbon-silicon copolymer, a hydrophobic filler, an organo-silicone surfactant, a hydrocarbon carrier oil, and, optionally, a silicone oil are disclosed in Kulcarni et al U.S. Pat. No. 4,514,319.
Fluid antifoaming or defoaming compositions comprising mineral oil-containing dispersed hydrophobic solid particles are well known in the art. The use of hydrophobic silica in fluid hydrocarbon oil based antifoam or defoaming compositions is disclosed in U.S. Pat. Nos. 3,076,768; 3,207,698; 3,388,073; and 3,714,068.
Fluid antifoaming or de foaming compositions comprising polyoxyethylene-polypropylene copolymers containing dispersed hydrophobic silica are disclosed in U.S. Pat. Nos 3,912,652 and 3,959,176.
Fluid antifoaming or defoaming compositions in a non-silicone oil and containing activated insitu hydrophobic silica particles are disclosed in U.S. Pat. No. 3,304,266.
Fluid antifoaming or de foaming compositions comprising a non-silicone water insoluble polyalkylene containing an alkoxysilicon chloride as the hydrophobic agent are disclosed in G.B. Pat. No. 1,166,877.
Fluid antifoaming or defoaming compositions employing the use of other intrinsically hydrophobic fillers in organic liquids are also well known. For example, Canadian Pat. No. 508,856 discloses N,N'-distearyl ethylene-diamide in white spirits, while the use of finely divided polyolefin polymers or polyesters dispersed in organic liquids is disclosed in U.S. Pat. No. 3,705,859. The use of fatty acid salts is disclosed in G.B. Pat. No. 1,267,482 and low molecular weight polyethylenes in combination with mineral oil and conventional organic nonionic emulsifiers is disclosed in U.S. Pat. No. 3,909,445.
Fluid antifoam or defoaming compositions comprising silicone oil-silica compounds containing organo silicone compounds to improve performance are disclosed in U.S. Pat. No. 3,691,091.
Fluid antifoam or defoaming compositions comprising the use of silicone-glycol copolymers in association with silicone oil and silica are disclosed in U.S. Pat. Nos. 3,746,653; 3,784,479; and 3,865,544.
Simethecone is a fluid antifoam or defoaming composition comprised of polydimethylsiloxane and silica suitably purified for its intended application. The preparation of liquid methylsiloxane polymers is delineated in U.S. Pat. No. 2,441,098, the disclosure of which is hereby incorporated by reference. The normal physical state of the simethicone is a water white to grey translucent, viscous, oil-like liquid with a density of 0.965-0.970 grams/cubic centimeter having demonstrable immiscibility with water and alcohol.
The medically established therapeutic use for simethicone is as an ointment base ingredient, topical drug vehicle, skin protectant, but most particularly as an antigas and antiflatulent agent for human application as well as an antibloating agent for veterinary (animal) application. A combinate of simethicone and calcium silicate useful for such latter applications is disclosed in Valentine et al. U.S. Pat. No. 4,906,478.
Various antigas or antifoam formulations, some containing simethicone, are disclosed in the prior art. The pharmaceutical and medicinal applications include Buehler et al U.S. Pat. No. 4,605,551; Prussin et al U.S. Pat. No. 3,326,754; Thompson et al U.S. Pat. No. 2,774,710; Rubino et al U.S. Pat. No. 4,115,553; Mitra U.S. Pat. No. 4,396,604; McVean et al U.S. Pat. No. 3,767,794; and Morris et al. U.S. Pat. No. 4,581,381. Non-pharmaceutical and non-medicinal antifoaming applications, such as powdered cleaning agents, are disclosed in Farminer et al U.S. Pat. No. 3,843,558; Llenado U.S. Pat. No. 4,180,485; Abel U.S. Pat. No. 4,264,465; Matheson et al U.S. Pat. No. 4,102,823; and European Patent 213,953 to Iley et al.
The preferred pharmaceutical solid dose delivery system for simethicone is a chewable tablet Such chewable tablets often contain antacid ingredients such as calcium carbonate, aluminum hydroxide, magnesium hydroxide and magnesium carbonate. The article by F. Maksond et al, "Simethicone use in Antacid Medications" as published in Manufacturing Chemist and Aerosol News, Vol. 47, No. 5, 1976, pp 36-36 discloses instability problems when simethicone is intermixed with aluminum or magnesium bases It is extremely troublesome to distribute the oil-like, viscous, water and alcohol immiscible simethicone expeditiously and uniformly throughout a tablet granulation prior to compression. It is equally difficult to be certain that the simethicone is in a sufficiently divided and dispersed state so that its action will be quick and effective when administered per os as a chewable or swallowable tablet or powder filled capsule.
Similar problems are encountered in distributing the other anitfoaming compositions in an expeditious and uniform manner in their liquid form.
Bearing in mind the problems and deficiencies of the prior art, it is therefore an object of the present invention to provide an improved dry, granular combinate for dispersing liquid antifoaming or defoaming compounds in an aqueous medium.
It is another object of the present invention to provide an effective simethicone containing granule for use in gastric antacid, antigas, and/or antiflatulent formulations.
It is a further object of the present invention to provide granules to be added to aqueous based products or processes wherever antifoaming or defoaming is indicated or desired.
It is yet another object of the present invention to provide a facile method of producing an effective simethicone-containing foam controlling granule utilizing conventional equipment at relatively low cost.
It is a further object of the present invention to provide a free flowing simethicone containing granule for use in conventional formulations which, after processing, retains acceptable defoaming activity.
It is yet another object of the present invention to provide an antifoaming or defoaming compound combinate which retains its properties and activity after extended storage and at elevated temperatures.
The present invention achieves these objects and satisfies the long felt need to overcome the difficulties in expeditious utilization of antifoaming or defoaming compounds in an aqueous medium A larger amount of antifoaming or defoaming compound can be incorporated with the carbohydrate-based agglomerate of this invention for dispersion than has previously been disclosed in the prior art. The carbohydrate-based agglomerate portion of the combinate makes it possible to effect rapid and uniform distribution of the antifoaming/defoaming compound by simple mixing.